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Quinoline carboxamide-type ABCG2 modulators: Indole and quinoline moieties as anilide replacements

Bauer, Stefanie ; Ochoa Puentes, Cristian ; Sun, Qiu ; Bause, Manuel ; Bernhardt, Günther ; König, Burkhard ; Buschauer, Armin


Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent ABCG2 modulators reported so far.

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